| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
PF-06726304 is a novel, potent and selective SAM-competitive EZH2 (enhancer of zeste homolog 2) inhibitor with a Ki of 0.7 nM. PF-06726304 displayed improved LipE and on-target potency in both biochemical and cellular readouts relative to compound 18. PF-06726304 also displayed robust in vivo antitumor growth activity and dose-dependent de-repression of EZH2 target genes.
| ln Vitro |
PF-06726304 (Compound 31) inhibits Karpas-422 H3K27me3 with an IC50 of 15 nM [1]. PF-06726304, with an IC50 of 25 nM, suppresses the growth of Karpas-422 cells carrying wild-type EZH2[1].
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| ln Vivo |
In a subcutaneous Karpas-422 xenograft model, PF-06726304 (200 and 300 mg/kg; BID 20 days) suppresses tumor development and causes a strong modification of downstream indicators [1].
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| Animal Protocol |
Animal/Disease Models: Female Scid beige mice (6-8 weeks old) using Karpas-422 xenograft model [1]
Doses: 200 and 300 mg/kg Route of Administration: BID for 20 days Experimental Results: Inhibited tumor growth and induced downstream organisms Robust modulation of markers in a subcutaneousKarpas-422 xenograft model. |
| References |
| Molecular Formula |
C22H21CL2N3O3
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|---|---|
| Molecular Weight |
446.326443433762
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| Exact Mass |
445.095
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| CAS # |
1616287-82-1
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| Related CAS # |
PF-06726304 acetate;2080306-28-9
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| PubChem CID |
86723730
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| Appearance |
White to off-white solid powder
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| LogP |
3.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
799
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(=O)C2=C(C(Cl)=CC(C3=C(C)ON=C3C)=C2Cl)CCN1CC1=C(C)C=C(C)NC1=O
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| InChi Key |
PDKDOPJQPKXNCT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H21Cl2N3O3/c1-10-7-11(2)25-21(28)16(10)9-27-6-5-14-17(23)8-15(20(24)19(14)22(27)29)18-12(3)26-30-13(18)4/h7-8H,5-6,9H2,1-4H3,(H,25,28)
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| Chemical Name |
5,8-Dichloro-2-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-7-(3,5-dimethyl-4-isoxazolyl)-3,4-dihydro-1(2H)-isoquinolinone
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| Synonyms |
PF-6726304; PF 6726304; PF6726304; PF-06726304; PF 06726304; PF06726304;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 15 mg/mL (~33.61 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.24 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (2.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2405 mL | 11.2025 mL | 22.4049 mL | |
| 5 mM | 0.4481 mL | 2.2405 mL | 4.4810 mL | |
| 10 mM | 0.2240 mL | 1.1202 mL | 2.2405 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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